RS50737B - Beta-amino tetrahydroimidazo (1,2-a)pyrazines and tetrahydrotrioazolo (4,3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes - Google Patents

Beta-amino tetrahydroimidazo (1,2-a)pyrazines and tetrahydrotrioazolo (4,3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

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Publication number
RS50737B
RS50737B YUP-1006/03A YUP100603A RS50737B RS 50737 B RS50737 B RS 50737B YU P100603 A YUP100603 A YU P100603A RS 50737 B RS50737 B RS 50737B
Authority
RS
Serbia
Prior art keywords
6alkyl
substituted
unsubstituted
linear
pyrazines
Prior art date
Application number
YUP-1006/03A
Other languages
Serbian (sr)
Inventor
Scott D. Edmondson
Michael H. Fisher
Dooseop Kim
Malcolm Maccoss
Emma R. Parmee
Ann E. Weber
Jinyou Xu
Original Assignee
Merck Sharp & Dohme Corp.
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Application filed by Merck Sharp & Dohme Corp. filed Critical Merck Sharp & Dohme Corp.
Publication of YU100603A publication Critical patent/YU100603A/en
Publication of RS50737B publication Critical patent/RS50737B/en

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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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Abstract

Jedinjenje formule I:naznačeno time što:Ar je fenil koji je nesupstituisan ili supstituisan sa 1-5 R3, pri čemu je R3 nezavisno izabran iz grupe koju čine:(1) halogen,(2) C1-6alkil, koji je linearan ili granat i nesupstituisan ili supstituisan sa 1-5 halogena,(3) OC1-6alkil, koji je linearan ili granat i nesupstituisan ili supstituisan sa 1-5 halogena, i(4) CN;X je izabran iz grupe koju čine:(l)N,i (2) CR2;R1 i R2 su nezavisno izabrani iz grupe koju čine:(1) vodonik,(2) CN,(3) C1-10alkil, koji je linearan ili granat i koji je nesupstituisan ili supstituisan sa 1-5 halogena, ili fenil, koji je nesupstituisan ili supstituisan sa 1-5 supstituenata nezavisno izabranih od halogena, CN, OH, R4, OR4, NHSO2R4, SO2R4, CO2H i CO2C1-6alkil, pri čemu je CO2C1-6alkil linearan ili granat,(4) fenil koji je nesupstituisan ili supstituisan sa 1-5 supstituenata nezavisno izabranih od halogena, CN, OH, R4, OR4, NHSO2R4, SO2R4, CO2H i CO2C1-6alkil, pri čemu je CO2C1-6alkil linearan ili granat, i(5) 5- ili 6-člani heterocikl . koji može biti zasićen ili nezasićen i koji sadrži 1-4 heteroatoma nezavisno izabranih od N, S i O, pri čemu je heterocikl nesupstituisan ili supstituisan sa 1-3 supstituenta nezavisno izabranih od okso, OH, halogena, C1-6alkil i OC1-6alkil, pri čemu su C1-6alkil i OC1-6alkil linearni ili granati i izborno supstituisani sa 1-5 halogena;R4 je C1-6alkil, koji je linearan ili granat i koji je nesupstituisan ili supstituisan sa 1-5 grupa nezavisno izabranih od halogena, CO2H i CO2C1-6alkil, pri čemu je CO2C1-6alkil linearan ili granat;i njegove farmaceutski prihvatljive soli i pojedinačni diastereomeri. Prijava sadrži još 29 zavisnih patentnih zahteva.Compound of Formula I: wherein: Ar is phenyl which is unsubstituted or substituted with 1-5 R3, wherein R3 is independently selected from the group consisting of: (1) halogen, (2) C1-6alkyl, which is linear or garnet and unsubstituted or substituted with 1-5 halogens, (3) OC1-6alkyl, which is linear or garnet and unsubstituted or substituted with 1-5 halogens, and (4) CN; X is selected from the group consisting of: (l) N , and (2) CR2; R1 and R2 are independently selected from the group consisting of: (1) hydrogen, (2) CN, (3) C1-10alkyl, which is linear or garnet and which is unsubstituted or substituted by 1-5 halogen, or phenyl, which is unsubstituted or substituted by 1-5 substituents independently selected from halogen, CN, OH, R4, OR4, NHSO2R4, SO2R4, CO2H and CO2C1-6alkyl, wherein CO2C1-6alkyl is linear or garnet, (4 ) phenyl which is unsubstituted or substituted by 1-5 substituents independently selected from halogen, CN, OH, R4, OR4, NHSO2R4, SO2R4, CO2H and CO2C1-6alkyl, wherein CO2C1-6alkyl is linear or garnet, and (5 ) 5- or 6-membered heterocycle. which may be saturated or unsaturated and containing 1-4 heteroatoms independently selected from N, S and O, wherein the heterocycle is unsubstituted or substituted with 1-3 substituents independently selected from oxo, OH, halogen, C1-6alkyl and OC1-6alkyl , wherein C1-6alkyl and OC1-6alkyl are linear or garnets and optionally substituted with 1-5 halogens; R4 is C1-6alkyl, which is linear or garnet and which is unsubstituted or substituted with 1-5 groups independently selected from halogen, CO2H and CO2C1-6alkyl, wherein CO2C1-6alkyl is linear or garnet; and its pharmaceutically acceptable salts and individual diastereomers. The application contains another 29 dependent claims.

YUP-1006/03A 2001-07-06 2002-07-05 Beta-amino tetrahydroimidazo (1,2-a)pyrazines and tetrahydrotrioazolo (4,3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes RS50737B (en)

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Application Number Priority Date Filing Date Title
US30347401P 2001-07-06 2001-07-06

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YU100603A YU100603A (en) 2006-05-25
RS50737B true RS50737B (en) 2010-08-31

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Families Citing this family (428)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020006899A1 (en) * 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
US7544511B2 (en) * 1996-09-25 2009-06-09 Neuralstem Biopharmaceuticals Ltd. Stable neural stem cell line methods
US20030176357A1 (en) * 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
CZ20012358A3 (en) * 1998-12-31 2002-01-16 Societe De Conseils De Recherches Et D´Application Prenyltransferase inhibitors
CA2450579A1 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
EP1406622B1 (en) 2001-06-20 2006-02-22 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
KR20040015298A (en) 2001-06-27 2004-02-18 스미스클라인 비참 코포레이션 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
UA74912C2 (en) * 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
WO2003068805A2 (en) * 2002-02-14 2003-08-21 Bayer Pharmaceuticals Corporation Formulation strategies in stabilizing peptides in organic solvents and in dried states
WO2003082817A2 (en) * 2002-03-25 2003-10-09 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
WO2004007468A1 (en) * 2002-07-15 2004-01-22 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
WO2004032836A2 (en) * 2002-10-07 2004-04-22 Merck & Co., Inc. Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors
JP4352001B2 (en) * 2002-10-18 2009-10-28 メルク エンド カムパニー インコーポレーテッド Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
ES2278213T3 (en) 2002-11-07 2007-08-01 MERCK & CO., INC. PHENYLAMINE DERIVATIVES AS INHIBITORS OF DIPEPTIDILPEPTIDASA IN THE TREATMENT OR PREVENTION OF DIABETES.
CA2508487A1 (en) * 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20040185429A1 (en) 2002-12-09 2004-09-23 Judith Kelleher-Andersson Method for discovering neurogenic agents
US8293488B2 (en) 2002-12-09 2012-10-23 Neuralstem, Inc. Method for screening neurogenic agents
BR0317028A (en) * 2002-12-10 2005-10-25 Novartis Ag Combination of a dpp-iv inhibitor and a ppar-alpha compound
CA2508947A1 (en) * 2002-12-20 2004-07-15 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US8293751B2 (en) 2003-01-14 2012-10-23 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
US7265128B2 (en) * 2003-01-17 2007-09-04 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
EP1592689A4 (en) * 2003-01-31 2008-12-24 Merck & Co Inc 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AR043443A1 (en) * 2003-03-07 2005-07-27 Merck & Co Inc PROCEDURE FOR THE PREPARATION OF TETRAHYDROTRIAZOLOPIRAZINS AND INTERMEDIATE PRODUCTS
AR043505A1 (en) * 2003-03-18 2005-08-03 Merck & Co Inc PREPARATION OF BETA-CETOAMIDS AND REACTION INTERMEDIARIES
AR043515A1 (en) * 2003-03-19 2005-08-03 Merck & Co Inc PROCEDURE TO PREPARE CHIRAL DERIVATIVES BETA AMINO ACIDS BY ASYMMETRIC HYDROGENATION
WO2004085661A2 (en) * 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
US7550590B2 (en) * 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2004087650A2 (en) * 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors
JP4806628B2 (en) 2003-05-05 2011-11-02 プロビオドルグ エージー Glutaminyl cyclase inhibitor
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2004103276A2 (en) 2003-05-14 2004-12-02 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1635832A2 (en) * 2003-06-06 2006-03-22 Merck & Co., Inc. Combination therapy for the treatment of diabetes
CN1798556A (en) * 2003-06-06 2006-07-05 麦克公司 Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004112701A2 (en) * 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JO2625B1 (en) * 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
AR045047A1 (en) 2003-07-11 2005-10-12 Arena Pharm Inc ARILO AND HETEROARILO DERIVATIVES TRISUSTITUIDOS AS MODULATORS OF METABOLISM AND PROFILAXIS AND TREATMENT OF DISORDERS RELATED TO THEMSELVES
WO2005007658A2 (en) 2003-07-14 2005-01-27 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
SI1648933T1 (en) * 2003-07-25 2010-01-29 Conjuchem Biotechnologies Inc Long lasting insulin derivatives and methods thereof
WO2005011581A2 (en) * 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
ZA200602051B (en) * 2003-08-13 2007-10-31 Takeda Pharmaceutical 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors
JP2007504230A (en) * 2003-09-02 2007-03-01 メルク　エンド　カムパニー　インコーポレーテッド A novel crystalline form of phosphate of dipeptidyl peptidase-IV inhibitor
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
JP2007513058A (en) * 2003-09-08 2007-05-24 武田薬品工業株式会社 Dipeptidyl peptidase inhibitor
CN1902177A (en) 2003-09-22 2007-01-24 万有制药株式会社 Novel piperidine derivative
EP1667524A4 (en) * 2003-09-23 2009-01-14 Merck & Co Inc Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
US20070123470A1 (en) * 2003-10-24 2007-05-31 Wladimir Hogenhuis Enhancement of growth hormone levels with a dipeptidyl peptidase IV inhibitor and a growth hormone secretagogue
EP2338490A3 (en) 2003-11-03 2012-06-06 Probiodrug AG Combinations useful for the treatment of neuronal disorders
US7238683B2 (en) * 2003-11-04 2007-07-03 Merck & Co., Inc. Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
PL1689757T3 (en) * 2003-11-12 2015-05-29 Sino Med Int Alliance Inc Heterocyclic boronic acid compounds
US7767828B2 (en) * 2003-11-12 2010-08-03 Phenomix Corporation Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7317109B2 (en) * 2003-11-12 2008-01-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7576121B2 (en) * 2003-11-12 2009-08-18 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
KR20170005163A (en) 2003-11-17 2017-01-11 노파르티스 아게 Use of dipeptidyl peptidase iv inhibitors
WO2005072530A1 (en) * 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
EP2165703A3 (en) 2004-01-20 2012-03-28 Novartis Pharma AG Direct compression formulation and process
BRPI0507485A (en) 2004-02-05 2007-07-10 Probiodrug Ag new glutaminyl cyclase inhibitors
AU2005210285B2 (en) * 2004-02-05 2008-01-24 Kyorin Pharmaceutical Co., Ltd. Bicycloester derivative
CN1922139B (en) * 2004-02-18 2010-12-29 杏林制药株式会社 Bicyclic amide derivatives
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
JP4689599B2 (en) * 2004-02-27 2011-05-25 杏林製薬株式会社 Bicyclo derivative
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
CN102127053A (en) 2004-03-15 2011-07-20 武田药品工业株式会社 Dipeptidyl peptidase inhibitors
CN1938286A (en) 2004-03-29 2007-03-28 默克公司 Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
EP1734963A4 (en) 2004-04-02 2008-06-18 Merck & Co Inc Method of treating men with metabolic and anthropometric disorders
TW200602293A (en) * 2004-04-05 2006-01-16 Merck & Co Inc Process for the preparation of enantiomerically enriched beta amino acid derivatives
CA2564264A1 (en) * 2004-05-04 2005-11-17 Merck & Co., Inc. 1,2,4-oxadiazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CA2564884A1 (en) * 2004-05-18 2005-12-08 Merck & Co., Inc. Cyclohexylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US7687638B2 (en) * 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
CN101014598B (en) * 2004-06-21 2012-06-13 默沙东公司 Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
ATE553077T1 (en) * 2004-07-23 2012-04-15 Nuada Llc PEPTIDATE INHIBITORS
TW200608967A (en) 2004-07-29 2006-03-16 Sankyo Co Pharmaceutical compositions containing with diabetic agent
US7915252B2 (en) 2004-08-06 2011-03-29 Merck Sharp & Dohme Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
CA2576465A1 (en) * 2004-08-23 2006-03-02 Merck & Co., Inc. Fused triazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US20070259927A1 (en) * 2004-08-26 2007-11-08 Takeda Pharmaceutical Company Limited Remedy for Diabetes
AR050615A1 (en) 2004-08-27 2006-11-08 Novartis Ag PHARMACEUTICAL COMPOSITIONS FOR ORAL ADMINISTRATION
WO2006033848A1 (en) * 2004-09-15 2006-03-30 Merck & Co., Inc. Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
US20060063719A1 (en) * 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
EP1796669B1 (en) 2004-10-01 2010-09-22 Merck Sharp & Dohme Corp. Aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
MX2007004305A (en) * 2004-10-12 2007-06-18 Glenmark Pharmaceuticals Sa Novel dipeptidyl peptidase iv inhibitors, pharmaceutical compositions containing them, and process for their preparation.
DE102004054054A1 (en) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Process for preparing chiral 8- (3-amino-piperidin-1-yl) -xanthines
IN2014CN03629A (en) * 2004-11-17 2015-09-04 Neuralstem Inc
US7872124B2 (en) 2004-12-21 2011-01-18 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DOP2006000008A (en) * 2005-01-10 2006-08-31 Arena Pharm Inc COMBINED THERAPY FOR THE TREATMENT OF DIABETES AND RELATED AFFECTIONS AND FOR THE TREATMENT OF AFFECTIONS THAT IMPROVE THROUGH AN INCREASE IN THE BLOOD CONCENTRATION OF GLP-1
BRPI0609371A2 (en) 2005-03-08 2010-03-30 Nycomed Gmbh uses of roflumilast in the production of pharmaceutical compositions for the treatment of diabetes mellitus
TWI357902B (en) 2005-04-01 2012-02-11 Lg Life Science Ltd Dipeptidyl peptidase-iv inhibiting compounds, meth
CA2606188A1 (en) * 2005-05-02 2006-11-09 Merck & Co., Inc. Combination of dipeptidyl peptidase-iv inhibitor and a cannabinoid cb1 receptor antagonist for the treatment of diabetes and obesity
CN101500573A (en) * 2005-05-25 2009-08-05 默克公司 Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US7825139B2 (en) * 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
RU2417985C2 (en) 2005-05-30 2011-05-10 Баниу Фармасьютикал Ко., Лтд. Novel piperidine derivatives
MY152185A (en) 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
JP4915833B2 (en) * 2005-07-01 2012-04-11 雪印メグミルク株式会社 Dipeptidyl peptidase IV inhibitor
ES2426345T3 (en) * 2005-07-20 2013-10-22 Eli Lilly And Company Compound bound in 1-amino position
ES2391470T3 (en) 2005-07-20 2012-11-27 Eli Lilly And Company Phenyl compounds
ES2325558T3 (en) 2005-07-20 2009-09-08 Eli Lilly And Company PIRIDINE DERIVATIVES AS INHIBITORS OF DIPEPTIDILPEPTIDASA.
EP1909776A2 (en) * 2005-07-25 2008-04-16 Merck & Co., Inc. Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor
DE102005035891A1 (en) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8- (3-amino-piperidin-1-yl) -xanthines, their preparation and their use as pharmaceuticals
CA2618112A1 (en) 2005-08-10 2007-02-15 Banyu Pharmaceutical Co., Ltd. Pyridone compound
AU2006282260A1 (en) 2005-08-24 2007-03-01 Msd K.K. Phenylpyridone derivative
WO2007028051A2 (en) 2005-09-02 2007-03-08 Abbott Laboratories Novel imidazo based heterocycles
EP1939194A4 (en) 2005-09-07 2010-12-08 Banyu Pharma Co Ltd Bicyclic aromatic substituted pyridone derivative
DK1942898T4 (en) 2005-09-14 2014-06-02 Takeda Pharmaceutical Dipeptidyl peptidase inhibitors for the treatment of diabetes
PL1931350T5 (en) * 2005-09-14 2021-11-15 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
TW200745080A (en) * 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor
TW200745079A (en) * 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor
KR101368988B1 (en) 2005-09-16 2014-02-28 다케다 야쿠힌 고교 가부시키가이샤 Dipeptidyl peptidase inhibitors
BRPI0616463A2 (en) 2005-09-29 2011-06-21 Merck & Co Inc compound, pharmaceutical composition, and use of a compound
TW200738266A (en) * 2005-09-29 2007-10-16 Sankyo Co Pharmaceutical agent containing insulin resistance improving agent
US20090156579A1 (en) * 2005-10-25 2009-06-18 Hasegawa Philip A Combination of a Dipeptidyl Peptidase-4 Inhibitor and an Anti-Hypertensive Agent for the Treatment of Diabetes and Hypertension
AU2006307046A1 (en) 2005-10-27 2007-05-03 Msd K.K. Novel benzoxathiin derivative
BRPI0620718A2 (en) * 2005-10-28 2011-11-22 Takeda Pharmaceutical agent for the protection of the pancreas, and, use of a glucose-lowering drug
NZ568292A (en) 2005-11-10 2011-08-26 Msd Kk Spiro[cyclohexane-1,1'-(3'H)-4'-azaisobenzofuran]-4-carboxamide derivatives
EP1801098A1 (en) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors
CN101365432B (en) * 2005-12-16 2011-06-22 默沙东公司 Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
US20100222393A1 (en) * 2005-12-30 2010-09-02 Naresh Kumar Muscarinic receptor antagonists
US20090156465A1 (en) 2005-12-30 2009-06-18 Sattigeri Jitendra A Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors
AU2007208405B2 (en) * 2006-01-25 2011-05-26 Merck Sharp & Dohme Corp. Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
JP5101489B2 (en) * 2006-03-08 2012-12-19 杏林製薬株式会社 Process for producing aminoacetylpyrrolidinecarbonitrile derivative and its production intermediate
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP2009531456A (en) * 2006-03-28 2009-09-03 武田薬品工業株式会社 Preparation of (R) -3-aminopiperidine dihydrochloride
PE20071221A1 (en) 2006-04-11 2007-12-14 Arena Pharm Inc GPR119 RECEPTOR AGONISTS IN METHODS TO INCREASE BONE MASS AND TO TREAT OSTEOPOROSIS AND OTHER CONDITIONS CHARACTERIZED BY LOW BONE MASS, AND COMBINED THERAPY RELATED TO THESE AGONISTS
EP2369341A3 (en) * 2006-04-11 2012-01-04 Arena Pharmaceuticals, Inc. Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual
AU2007236115A1 (en) 2006-04-11 2007-10-18 Novartis Ag Organic compounds
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
NO347644B1 (en) 2006-05-04 2024-02-12 Boehringer Ingelheim Int Polymorphs
PE20080251A1 (en) 2006-05-04 2008-04-25 Boehringer Ingelheim Int USES OF DPP IV INHIBITORS
NZ574710A (en) 2006-09-07 2012-02-24 Nycomed Gmbh Combination treatment comprising the PDE4 inhibitor Compound A ((2R,4aR, 10bR)6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1 ,2,3,4,4a,10b-hexahydrophenanthridin-2-ol) for diabetes mellitus
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
PE20081150A1 (en) * 2006-09-13 2008-10-03 Takeda Pharmaceutical DIPETHYLPEPTIDASE INHIBITORS
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
JPWO2008038692A1 (en) 2006-09-28 2010-01-28 萬有製薬株式会社 Diaryl ketimine derivatives
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
TW200838536A (en) * 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
ATE554085T1 (en) 2006-11-30 2012-05-15 Probiodrug Ag NEW INHIBITORS OF GLUTAMINYL CYCLASE
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
KR20080071476A (en) * 2007-01-30 2008-08-04 주식회사 엘지생명과학 Novel dipeptidyl peptidase-iv inhibitors
PL2107905T3 (en) * 2007-02-01 2011-04-29 Takeda Pharmaceuticals Co Solid preparation comprising alogliptin and pioglitazone
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US20070172525A1 (en) * 2007-03-15 2007-07-26 Ramesh Sesha Anti-diabetic combinations
US20080064701A1 (en) * 2007-04-24 2008-03-13 Ramesh Sesha Anti-diabetic combinations
JPWO2008114857A1 (en) * 2007-03-22 2010-07-08 杏林製薬株式会社 Process for producing aminoacetylpyrrolidinecarbonitrile derivative
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
WO2008120813A1 (en) 2007-04-03 2008-10-09 Mitsubishi Tanabe Pharma Corporation Combined use of dipeptidyl peptidase iv inhibitor compound and sweetener
JP5667440B2 (en) 2007-04-18 2015-02-12 プロビオドルグ エージー Thiourea derivatives as glutaminyl cyclase inhibitors
AU2008248186B2 (en) 2007-05-07 2014-02-06 Merck Sharp & Dohme Corp. Method of treatment using fused aromatic compounds having anti-diabetic activity
WO2008141021A1 (en) * 2007-05-08 2008-11-20 Concert Pharmaceuticals, Inc. Deuterated derivatives of tetrahydrotriazolopyrazine compounds and their use as dpp-iv inhibitors
MX354786B (en) 2007-06-04 2018-03-21 Synergy Pharmaceuticals Inc AGONISTS OF GUANYLATE CYCLASE USEFUL FOR THE TREATMENT OF GASTROINTESTINAL DISORDERS, INFLAMMATION, CANCER and OTHER DISORDERS.
CA2690004C (en) 2007-06-04 2018-01-23 Ben-Gurion University Of The Negev Research And Development Authority Tri-aryl compounds and compositions comprising the same
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CN101318922B (en) * 2007-06-08 2010-11-10 上海阳帆医药科技有限公司 Novel dipeptidyl peptidase restrainer, synthesizing process and uses thereof
CL2008002427A1 (en) 2007-08-16 2009-09-11 Boehringer Ingelheim Int Pharmaceutical composition comprising 1-chloro-4- (bd-glucopyranos-1-yl) -2- [4 - ((s) -tetrahydrofuran-3-yloxy) benzyl] -benzene combined with 1 - [(4-methylquinazolin- 2-yl) methyl] -3-methyl-7- (2-butyn-1-yl) -8- (3- (r) -aminopiperidin-1-yl) xanthine; and its use to treat type 2 diabetes mellitus.
WO2009024542A2 (en) * 2007-08-17 2009-02-26 Boehringer Ingelheim International Gmbh Purin derivatives for use in the treatment of fab-related diseases
CN101397300B (en) * 2007-09-04 2011-04-27 山东轩竹医药科技有限公司 Dipeptidase-IV inhibitor derivates
US20090076013A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched sitagliptin
CN101417999A (en) * 2007-10-25 2009-04-29 上海恒瑞医药有限公司 Piperazines derivates, preparation method thereof and application thereof in medicine
WO2009084024A2 (en) * 2007-11-02 2009-07-09 Glenmark Generics Limited A process for the preparation of r-sit agliptin and its pharmaceutically acceptable salts thereof
US20090192326A1 (en) * 2007-11-13 2009-07-30 Nurit Perlman Preparation of sitagliptin intermediate
EP2599781A1 (en) 2007-12-20 2013-06-05 Dr. Reddy's Laboratories Ltd. Processes for the preparation of sitagliptin and pharmaceutically acceptable salts thereof
CN101903386B (en) 2007-12-21 2015-04-22 株式会社Lg生命科学 Dipeptidyl peptidase-IV inhibiting compounds, methods of preparing the same, and pharmaceutical compositions containing the same as active agent
CN101468988A (en) 2007-12-26 2009-07-01 上海恒瑞医药有限公司 Piperazine derivative, preparation thereof and use thereof in medicine
CL2008003653A1 (en) 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Use of a glucopyranosyl-derived sglt inhibitor and a selected dppiv inhibitor to treat diabetes; and pharmaceutical composition.
PE20091353A1 (en) 2008-01-24 2009-09-05 Panacea Biotec Ltd NEW HETEROCYCLIC COMPOUNDS
AU2009210641A1 (en) * 2008-02-05 2009-08-13 Merck Sharp & Dohme Corp. Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-IV inhibitor
AU2009220444A1 (en) * 2008-03-04 2009-09-11 Merck Sharp & Dohme Corp. Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-IV inhibitor
CA2714617A1 (en) 2008-03-06 2009-09-11 Banyu Pharmaceutical Co., Ltd. Alkylaminopyridine derivative
US8551524B2 (en) * 2008-03-14 2013-10-08 Iycus, Llc Anti-diabetic combinations
US20090247532A1 (en) * 2008-03-28 2009-10-01 Mae De Ltd. Crystalline polymorph of sitagliptin phosphate and its preparation
US20110015198A1 (en) 2008-03-28 2011-01-20 Banyu Pharmaceutical Co., Inc. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
AR071175A1 (en) 2008-04-03 2010-06-02 Boehringer Ingelheim Int PHARMACEUTICAL COMPOSITION THAT INCLUDES AN INHIBITOR OF DIPEPTIDIL-PEPTIDASA-4 (DPP4) AND A COMPARING PHARMACO
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
US20090264476A1 (en) * 2008-04-18 2009-10-22 Mckelvey Craig CB-1 receptor modulator formulations
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
US8003672B2 (en) * 2008-04-21 2011-08-23 Merck Sharp & Dohme Corp. CB-1 receptor modulator formulations
PE20100156A1 (en) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int NAFLD TREATMENT
CA2726917C (en) 2008-06-04 2018-06-26 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2301936A1 (en) 2008-06-19 2011-03-30 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diarylketoxime derivative
KR20110038011A (en) 2008-07-03 2011-04-13 라티오팜 게엠베하 Crystalline salts of sitagliptin
WO2010009319A2 (en) 2008-07-16 2010-01-21 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
EP2324027B1 (en) * 2008-07-29 2016-02-24 Medichem, S.A. New crystalline salt forms of a 5,6,7,8-tetrahydro-1,2,4- triazolo[4,3-a]pyrazine derivative
EP2319841A1 (en) 2008-07-30 2011-05-11 Msd K.K. (5-membered)-(5-membered) or (5-membered)-(6-membered) fused ring cycloalkylamine derivative
KR20200118243A (en) 2008-08-06 2020-10-14 베링거 인겔하임 인터내셔날 게엠베하 Treatment for diabetes in patients inappropriate for metformin therapy
UY32030A (en) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "TREATMENT FOR DIABETES IN INAPPROPRIATE PATIENTS FOR THERAPY WITH METFORMIN"
WO2010016584A1 (en) * 2008-08-07 2010-02-11 杏林製薬株式会社 Process for production of bicyclo[2.2.2]octylamine derivative
CN102186474A (en) * 2008-08-14 2011-09-14 杏林制药株式会社 stable pharmaceutical composition
BRPI0917675A2 (en) 2008-08-15 2015-12-01 Boehringer Ingelheim Int wound healing organic compounds
EP2331545B1 (en) 2008-08-27 2013-10-02 Cadila Healthcare Limited Improved process for preparation of (2r)-4-oxo-4-[3- (trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin- 7(8h)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine&new impurities in preparation thereof
MX2011002558A (en) 2008-09-10 2011-04-26 Boehringer Ingelheim Int Combination therapy for the treatment of diabetes and related conditions.
JP2012504630A (en) 2008-10-03 2012-02-23 シェーリング コーポレイション Spiromidazolone derivatives as glucagon receptor antagonists
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
KR101054911B1 (en) * 2008-10-17 2011-08-05 동아제약주식회사 Pharmaceutical composition for the prevention and treatment of diabetes or obesity containing a compound that inhibits the activity of dipeptidyl peptidase-IV and other anti-diabetic or anti-obesity drugs as an active ingredient
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
EP2350010B1 (en) 2008-10-30 2014-03-26 Merck Sharp & Dohme Corp. Isonicotinamide orexin receptor antagonists
CN102271509A (en) 2008-10-31 2011-12-07 默沙东公司 Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
JP5514831B2 (en) 2008-11-17 2014-06-04 メルク・シャープ・アンド・ドーム・コーポレーション Substituted bicyclic amines for the treatment of diabetes
US8865729B2 (en) 2008-12-23 2014-10-21 Boehringer Ingelheim International Gmbh Salt forms of a xanthine compound
EP2381772B1 (en) * 2008-12-31 2016-08-24 Chiral Quest, Inc. Process and intermediates for the preparation of n-acylated-4-aryl beta-amino acid derivatives
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
US8404727B2 (en) * 2009-01-07 2013-03-26 Glenmark Pharmaceuticals S.A. Pharmaceutical composition that includes a dipeptidyl peptidase-IV inhibitor
CA2749301C (en) 2009-01-09 2019-06-11 Gopalan Balasubramanian Dipeptidyl peptidase iv inhibitors
AR075204A1 (en) 2009-01-29 2011-03-16 Boehringer Ingelheim Int DPP-4 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USEFUL TO TREAT METABOLIC DISEASES IN PEDIATRIC PATIENTS, PARTICULARLY MELLITUS DIABETES TYPE 2
EP2218721A1 (en) 2009-02-11 2010-08-18 LEK Pharmaceuticals d.d. Novel salts of sitagliptin
CN104906582A (en) 2009-02-13 2015-09-16 勃林格殷格翰国际有限公司 Pharmaceutical composition comprising a SGLT2 inhibitor, a DPP-IV inhibitor and optionally a further antidiabetic agent and uses thereof
CN106177958A (en) 2009-02-13 2016-12-07 勃林格殷格翰国际有限公司 Comprise DPP 4 inhibitor (BI 1356) and optionally combine the antidiabetic medicine of other antidiabetic drug
EP2223923A1 (en) 2009-02-25 2010-09-01 Esteve Química, S.A. Process for the preparation of a chiral beta aminoacid derivative and intermediates thereof
CN101824036A (en) * 2009-03-05 2010-09-08 上海恒瑞医药有限公司 Salt of tetrahydroimidazo [1,5-a] pyrazine derivative, preparation method and pharmaceutical application thereof
CN102378751B (en) 2009-03-30 2014-08-20 东亚St株式会社 Improved method for preparing dipeptidyl peptidase-iv inhibitor and intermediate
WO2010114292A2 (en) * 2009-03-30 2010-10-07 동아제약 주식회사 Improved method for manufacturing dipeptidyl peptidase-iv inhibitor and intermediate
CN101849944A (en) * 2009-03-31 2010-10-06 江苏恒瑞医药股份有限公司 Medicinal composition for treating type 2 diabetes
WO2010122578A2 (en) * 2009-04-20 2010-10-28 Msn Laboratories Limited Process for the preparation of sitagliptin and its intermediates
EP2430025A1 (en) * 2009-05-11 2012-03-21 Generics [UK] Limited Sitagliptin synthesis
CN101899047B (en) * 2009-05-26 2016-01-20 盛世泰科生物医药技术(苏州)有限公司 Be used for the treatment of as depeptidyl peptidase inhibitors or the beta-amino tetrahydrochysene pyrazine of prevent diabetes, tetrahydropyrimidine and tetrahydropyridine
CN101899048B (en) 2009-05-27 2013-04-17 上海恒瑞医药有限公司 Salt of (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1- carboxylic acid methyl ester
US8470773B2 (en) 2009-06-12 2013-06-25 Merck Sharp & Dohme Corp. Thiophenes as glucagon receptor antagonists, compositions, and methods for their use
IT1395596B1 (en) * 2009-06-30 2012-10-16 Dipharma Francis Srl PROCEDURE FOR THE PREPARATION OF SITAGLIPTIN
UY32776A (en) 2009-07-09 2011-02-28 Irm Llc IMIDAZOPIRAZINE COMPOUNDS REPLACED FOR THE TREATMENT OF PARASITARY DISEASES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND APPLICATION.
AR077642A1 (en) 2009-07-09 2011-09-14 Arena Pharm Inc METABOLISM MODULATORS AND THE TREATMENT OF DISORDERS RELATED TO THE SAME
CA2768577A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
EP2462943A4 (en) 2009-08-03 2014-11-05 Kaneka Corp Dipeptidyl peptidase-4 inhibitor
WO2011019538A1 (en) 2009-08-13 2011-02-17 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EA022485B1 (en) * 2009-08-13 2016-01-29 Сандоз Аг CRYSTALLINE COMPOUND OF 7-[(3R)-3-AMINO-1-OXO-4-(2,4,5-TRIFLUORPHENYL)BUTYL]-5,6,7,8-TETRAHYDRO-3-(TRIFLUORMETHYL)-1,2,4-TRIAZOLO[4,3-a]PYRAZINE
CA2771352A1 (en) 2009-09-02 2011-03-10 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
SG178953A1 (en) 2009-09-11 2012-04-27 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
EP2295083A1 (en) 2009-09-15 2011-03-16 Ratiopharm GmbH Pharmaceutical composition comprising active agents metformin and sitagliptin or vildagliptin
CN102030683B (en) * 2009-09-27 2013-07-31 浙江九洲药业股份有限公司 Sitagliptin intermediate and preparation method and application thereof
EP2308847B1 (en) 2009-10-09 2014-04-02 EMC microcollections GmbH Substituted pyridines as inhibitors of dipeptidyl peptidase IV and their application for the treatment of diabetes and related diseases
WO2011058193A1 (en) 2009-11-16 2011-05-19 Mellitech [1,5]-diazocin derivatives
AU2010323068B2 (en) 2009-11-27 2015-09-03 Boehringer Ingelheim International Gmbh Treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin
WO2011079778A1 (en) 2009-12-30 2011-07-07 China Shanghai Fochon Pharmaceutical Co Ltd 3-(3-aminopiperidin-1-yl)-5-oxo-1,2,4-triazine derivates as dipeptidyl peptidase iv(dpp-iv) inhibitors
KR101156587B1 (en) 2010-02-19 2012-06-20 한미사이언스 주식회사 Preparation method of sitagliptin and amine salt intermediate used therein
EP2538783B1 (en) 2010-02-22 2016-06-01 Merck Sharp & Dohme Corp. Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
AU2011226074B2 (en) 2010-03-10 2015-01-22 Vivoryon Therapeutics N.V. Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
CZ303113B6 (en) 2010-03-16 2012-04-11 Zentiva, K.S. Process for preparing sitagliptin
WO2011113947A1 (en) 2010-03-18 2011-09-22 Boehringer Ingelheim International Gmbh Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions
CA2800507A1 (en) 2010-03-31 2011-10-06 Teva Pharmaceuticals Industries Ltd. Solid state forms of sitagliptin salts
WO2011125011A1 (en) * 2010-04-05 2011-10-13 Cadila Pharmaceuticals Limited Novel hypoglycemic compounds
CN102918027A (en) 2010-04-06 2013-02-06 艾尼纳制药公司 Modulators of the gpr119 receptor and the treatment of disorders related thereto
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
WO2011135586A2 (en) 2010-04-28 2011-11-03 Sun Pharmaceutical Industries Ltd. Process for the preparation of chiral beta amino carboxamide derivatives
WO2011138421A1 (en) 2010-05-05 2011-11-10 Boehringer Ingelheim International Gmbh Combination therapy
WO2011146358A1 (en) 2010-05-21 2011-11-24 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
CN102260265B (en) 2010-05-24 2015-09-02 上海阳帆医药科技有限公司 Hexahydropyrrolo [3,4-b] pyrrole derivative, Its Preparation Method And Use
EP2576563B1 (en) * 2010-06-04 2016-05-11 LEK Pharmaceuticals d.d. A NOVEL SYNTHETIC APPROACH TO ß-AMINOBUTYRYL SUBSTITUTED COMPOUNDS
EP2392575A1 (en) 2010-06-04 2011-12-07 LEK Pharmaceuticals d.d. A novel synthetic approach to ß-aminobutyryl substituted compounds
EP2397141A1 (en) 2010-06-16 2011-12-21 LEK Pharmaceuticals d.d. Process for the synthesis of beta-amino acids and derivatives thereof
KR20190050871A (en) 2010-06-24 2019-05-13 베링거 인겔하임 인터내셔날 게엠베하 Diabetes therapy
EP2407469A1 (en) 2010-07-13 2012-01-18 Chemo Ibérica, S.A. Salt of sitagliptin
EP2423178A1 (en) 2010-07-28 2012-02-29 Chemo Ibérica, S.A. Process for the production of sitagliptin
US9540611B2 (en) 2010-07-28 2017-01-10 Neuralstem, Inc. Methods for treating and/or reversing neurodegenerative diseases and/or disorders
EP2418196A1 (en) * 2010-07-29 2012-02-15 IMTM GmbH Dual alanyl-aminopeptidase and dipeptidyl-peptidase IV inhibitors
WO2012024183A1 (en) 2010-08-18 2012-02-23 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US20130158265A1 (en) 2010-08-27 2013-06-20 Dhananjay Govind Sathe Sitagliptin, salts and polymorphs thereof
WO2012035549A2 (en) 2010-09-13 2012-03-22 Panacea Biotec Ltd An improved process for the synthesis of beta amino acid derivatives
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
BR112013008100A2 (en) 2010-09-22 2016-08-09 Arena Pharm Inc "gpr19 receptor modulators and the treatment of disorders related thereto."
US20130289276A1 (en) 2010-10-08 2013-10-31 Cadila Healthcare Limited Process for preparing an intermediate of sitagliptin via enzymatic conversion
WO2012049566A1 (en) 2010-10-14 2012-04-19 Japan Tobacco Inc. Combination therapy for use in treating diabetes
AR083878A1 (en) 2010-11-15 2013-03-27 Boehringer Ingelheim Int VASOPROTECTORA AND CARDIOPROTECTORA ANTIDIABETIC THERAPY, LINAGLIPTINA, TREATMENT METHOD
CN102485718B (en) 2010-12-03 2014-03-26 浙江海翔药业股份有限公司 Sitagliptin intermediate and its preparation method
WO2012078448A1 (en) 2010-12-06 2012-06-14 Schering Corporation Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
WO2012076973A2 (en) 2010-12-09 2012-06-14 Aurobindo Pharma Limited Novel salts of dipeptidyl peptidase iv inhibitor
TWI494313B (en) * 2010-12-29 2015-08-01 Jiangsu Hengrui Medicine Co Pharmaceutical composition for the treatment of type 2 diabetes in mammals including human beings
US11974971B2 (en) 2011-01-07 2024-05-07 Anji Pharmaceuticals Inc. Compositions and methods for treating metabolic disorders
US9572784B2 (en) 2011-01-07 2017-02-21 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
SG10201607085WA (en) * 2011-01-07 2016-10-28 Elcelyx Therapeutics Inc Chemosensory Receptor Ligand-Based Therapies
US9211263B2 (en) 2012-01-06 2015-12-15 Elcelyx Therapeutics, Inc. Compositions and methods of treating metabolic disorders
US11759441B2 (en) 2011-01-07 2023-09-19 Anji Pharmaceuticals Inc. Biguanide compositions and methods of treating metabolic disorders
US8796338B2 (en) 2011-01-07 2014-08-05 Elcelyx Therapeutics, Inc Biguanide compositions and methods of treating metabolic disorders
US9480663B2 (en) 2011-01-07 2016-11-01 Elcelyx Therapeutics, Inc. Biguanide compositions and methods of treating metabolic disorders
KR101290029B1 (en) 2011-01-20 2013-07-30 에스티팜 주식회사 Preparation method of intermediate of sitagliptin
MY191100A (en) 2011-01-31 2022-05-30 Cadila Healthcare Ltd Treatment for lipodystrophy
EP2677869B1 (en) 2011-02-25 2017-11-08 Merck Sharp & Dohme Corp. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
US9580471B2 (en) 2011-03-01 2017-02-28 Synergy Pharmaceuticals, Inc. Process of preparing guanylate cyclase C agonists
SG10201405403QA (en) * 2011-03-03 2014-11-27 Cadila Healthcare Ltd Novel salts of dpp-iv inhibitor
ES2570167T3 (en) 2011-03-16 2016-05-17 Probiodrug Ag Benzimidazole derivatives as glutaminyl cyclase inhibitors
SI2691083T1 (en) 2011-03-29 2017-12-29 Krka, D.D., Novo Mesto Pharmaceutical composition of sitagliptin
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
EP2508506A1 (en) 2011-04-08 2012-10-10 LEK Pharmaceuticals d.d. Preparation of sitagliptin intermediates
WO2012138845A1 (en) 2011-04-08 2012-10-11 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
US20140066369A1 (en) 2011-04-19 2014-03-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
KR101369584B1 (en) 2011-04-19 2014-03-06 일양약품주식회사 Phenyl-isoxazol derivatives and preparation process thereof
US20140051714A1 (en) 2011-04-22 2014-02-20 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
CN102757431B (en) * 2011-04-24 2016-03-30 浙江华海药业股份有限公司 A kind of novel method of synthesizing sitagliptin
ITMI20110765A1 (en) * 2011-05-05 2012-11-06 Chemo Iberica Sa PROCESS FOR SITAGLIPTINA PRODUCTION
US8524936B2 (en) 2011-05-18 2013-09-03 Milan Soukup Manufacturing process for sitagliptin from L-aspartic acid
US9359385B2 (en) * 2011-05-27 2016-06-07 Lek Pharmaceuticals D.D. Preparation of sitagliptin intermediates
EP2527320A1 (en) 2011-05-27 2012-11-28 LEK Pharmaceuticals d.d. Preparation of Sitagliptin Intermediates
US20140088124A1 (en) 2011-06-02 2014-03-27 Robert J. DeVita Imidazole derivatives
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
AR086675A1 (en) * 2011-06-14 2014-01-15 Merck Sharp & Dohme PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF INHIBITORS OF DIPEPTIDIL PEPTIDASA-4 WITH SIMVASTATIN
EP2720544B1 (en) 2011-06-16 2016-12-21 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment
EP2726075A4 (en) 2011-06-29 2014-11-19 Merck Sharp & Dohme Novel crystalline forms of a dipeptidyl peptidase-iv inhibitor
EP2726484A1 (en) 2011-06-29 2014-05-07 Ranbaxy Laboratories Limited Solid dispersions of sitagliptin and processes for their preparation
EP2726483A1 (en) 2011-06-30 2014-05-07 Ranbaxy Laboratories Limited Novel salts of sitagliptin
EP2729468A4 (en) 2011-07-05 2015-03-18 Merck Sharp & Dohme Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
KR101985384B1 (en) 2011-07-15 2019-06-03 베링거 인겔하임 인터내셔날 게엠베하 Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
SI2736909T1 (en) 2011-07-27 2017-08-31 Farma Grs, D.O.O. Process for the preparation of sitagliptin and its pharmaceutically acceptable salts
EP2753328A1 (en) 2011-09-07 2014-07-16 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Dpp-iv inhibitor formulations
WO2013048916A1 (en) 2011-09-30 2013-04-04 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
PL2578208T3 (en) 2011-10-06 2014-10-31 Sanovel Ilac Sanayi Ve Ticaret As DPP-IV inhibitor solid dosage formulations
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US9181256B2 (en) 2011-10-14 2015-11-10 Laurus Labs Private Ltd. Salts of sitagliptin, process for the preparation and pharmaceutical composition therefore
AR088352A1 (en) 2011-10-19 2014-05-28 Merck Sharp & Dohme ANTAGONISTS OF THE RECEIVER OF 2-PIRIDILOXI-4-NITRILE OREXINE
WO2013062838A1 (en) 2011-10-24 2013-05-02 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as gpr119 agonists
CN102603749B (en) * 2011-10-27 2017-02-08 浙江华海药业股份有限公司 Synthesis method of sitagliptin intermediate
WO2013065066A1 (en) 2011-11-02 2013-05-10 Cadila Healthcare Limited Processes for preparing 4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [l,2,41-triazolo[43-a]pyrazin-7(8h)-yl]-l-(2,4,5- trifluorophenyl)butan-2-amine
WO2013068328A1 (en) 2011-11-07 2013-05-16 Intervet International B.V. Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors
WO2013068439A1 (en) 2011-11-09 2013-05-16 Intervet International B.V. 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors
CA2855009C (en) 2011-11-15 2019-07-09 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds useful as gpr119 agonists
WO2013084210A1 (en) 2011-12-08 2013-06-13 Ranbaxy Laboratories Limited Amorphous form of sitagliptin salts
BR112014016808B1 (en) 2012-01-06 2022-01-11 Anji Pharma (Us) Llc USE OF A BIGUANIDE COMPOUND FOR THE MANUFACTURE OF A DRUG TO LOWER BLOOD GLUCOSE LEVELS AND FOR THE TREATMENT OF A DISORDER OF GLUCOSE METABOLISM
JP6175074B2 (en) 2012-01-06 2017-08-02 エルセリクス セラピューティクス インコーポレイテッド Compositions and methods for treating metabolic disorders
EP2615080A1 (en) 2012-01-12 2013-07-17 LEK Pharmaceuticals d.d. Preparation of Optically Pure ß-Amino Acid Type Active Pharmaceutical Ingredients and Intermediates thereof
EP2814485A4 (en) 2012-02-17 2015-08-26 Merck Sharp & Dohme Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
ES2421956B1 (en) 2012-03-02 2014-09-29 Moehs Ibérica S.L. NEW CRYSTAL FORM OF SITAGLIPTINA SULFATE
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
MX2014012465A (en) 2012-04-16 2015-01-12 Kaneq Pharma Inc Fused aromatic phosphonate derivatives as precursors to ptp-1b inhibitors.
TWI469785B (en) 2012-04-25 2015-01-21 Inovobiologic Inc Dietary fiber compositions for the treatment of metabolic disease
EP2849755A1 (en) 2012-05-14 2015-03-25 Boehringer Ingelheim International GmbH A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
EP2674432A1 (en) 2012-06-14 2013-12-18 LEK Pharmaceuticals d.d. New synthetic route for the preparation of ß aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha]pyrazin-7-yl compounds
EP2874626A4 (en) 2012-07-23 2016-03-23 Merck Sharp & Dohme Treating diabetes with dipeptidyl peptidase-iv inhibitors
US9315508B2 (en) 2012-07-23 2016-04-19 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-IV inhibitors
CA2880901A1 (en) 2012-08-02 2014-02-06 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CA2881050A1 (en) 2012-08-08 2014-02-13 Cipla Limited Process for the preparation of sitagliptin and intermediate compounds
CN102898387B (en) * 2012-09-26 2015-01-07 浙江工业大学 Channelized method for continuously producing N-[(2Z)-piperazine-2-subunit]-2, 2, 2-trifluoroacetyl hydrazine
TWI500613B (en) 2012-10-17 2015-09-21 Cadila Healthcare Ltd Novel heterocyclic compounds
CN103788070B (en) * 2012-10-26 2017-10-20 南京华威医药科技开发有限公司 The inhibitor class polymers of DPP 4
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
CZ306115B6 (en) * 2012-12-04 2016-08-10 Zentiva, K.S. Process for preparing derivatives of 3-amino-4-(2,4,5-trifluorophenyl)-butanoic acid
CN103319487B (en) * 2013-01-10 2015-04-01 药源药物化学（上海）有限公司 Preparation method of sitagliptin and intermediate of sitagliptin
EP2769712A1 (en) 2013-02-21 2014-08-27 Siegfried International AG Pharmaceutical formulation comprising DPP-IV inhibitor agglomerates and DPP-IV inhibitor particles
WO2014130608A1 (en) 2013-02-22 2014-08-28 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
WO2014127745A1 (en) * 2013-02-22 2014-08-28 成都先导药物开发有限公司 Dpp-iv-inhibiting compounds and intermediates thereof
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
EP2970384A1 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
IN2013MU00916A (en) 2013-03-20 2015-06-26 Cadila Healthcare Ltd
WO2014174524A1 (en) 2013-04-22 2014-10-30 Cadila Healthcare Limited A novel composition for nonalcoholic fatty liver disease (nafld)
EP3004053B1 (en) 2013-05-30 2021-03-24 Cadila Healthcare Limited A process for preparation of pyrroles having hypolipidemic hypocholesteremic activities
JP6606491B2 (en) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド Ultra high purity agonist of guanylate cyclase C, method for producing and using the same
WO2015001568A2 (en) * 2013-07-01 2015-01-08 Laurus Labs Private Limited Sitagliptin lipoate salt, process for the preparation and pharmaceutical composition thereof
TW201513857A (en) 2013-07-05 2015-04-16 Cadila Healthcare Ltd Synergistic compositions
IN2013MU02470A (en) 2013-07-25 2015-06-26 Cadila Healthcare Ltd
WO2015033357A2 (en) 2013-09-06 2015-03-12 Cadila Healthcare Limited An improved process for the preparation of pyrrole derivatives
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CZ2013842A3 (en) 2013-11-01 2015-05-13 Zentiva, K.S. Stable polymorph of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine with L-tartaric acid
KR20160094956A (en) 2013-11-05 2016-08-10 벤-구리온 유니버시티 오브 더 네게브 리서치 앤드 디벨럽먼트 어쏘러티 Compounds for the treatment of diabetes and disease complications arising from same
CN103626775B (en) * 2013-12-02 2015-05-20 南京华威医药科技开发有限公司 DPP-4 inhibitor with diazine structure
WO2015089809A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Antidiabetic substituted heteroaryl compounds
IN2014MU00212A (en) 2014-01-21 2015-08-28 Cadila Healthcare Ltd
US10065945B2 (en) 2014-01-24 2018-09-04 Merck Sharp & Dohme Corp. Isoquinoline derivatives as MGAT2 inhibitors
IN2014MU00651A (en) 2014-02-25 2015-10-23 Cadila Healthcare Ltd
WO2015128453A1 (en) 2014-02-28 2015-09-03 Boehringer Ingelheim International Gmbh Medical use of a dpp-4 inhibitor
WO2015145333A1 (en) 2014-03-26 2015-10-01 Sun Pharmaceutical Industries Limited Process for the preparation of sitagliptin and its intermediate
CA2945681A1 (en) * 2014-04-17 2015-10-22 Merck Sharp & Dohme Corp. Sitagliptin tannate complex
WO2015162506A1 (en) 2014-04-21 2015-10-29 Suven Life Sciences Limited Process for the preparation of sitagliptin and novel intermediates
WO2015170340A2 (en) * 2014-05-06 2015-11-12 Laurus Labs Private Limited Novel polymorphs of sitagliptin hydrochloride, processes for its preparation and pharmaceutical composition thereof
WO2015176267A1 (en) 2014-05-22 2015-11-26 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
JP6574474B2 (en) 2014-07-21 2019-09-11 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Process for producing chiral dipeptidyl peptidase-IV inhibitor
US10100042B2 (en) 2014-08-08 2018-10-16 Merck Sharp & Dohme Corp. [5,6]—fused bicyclic antidiabetic compounds
CN104140430B (en) * 2014-08-08 2016-07-13 广东东阳光药业有限公司 A kind of racemization method of isomer
US10968193B2 (en) 2014-08-08 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
EP3177282B1 (en) 2014-08-08 2021-10-06 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
GB201415598D0 (en) 2014-09-03 2014-10-15 Univ Birmingham Elavated Itercranial Pressure Treatment
WO2016046679A1 (en) * 2014-09-28 2016-03-31 Mohan M Alapati Compositions and methods for the treatment of diabetes and pre-diabetes
CA2964927C (en) 2014-10-20 2019-07-30 Neuralstem, Inc. Stable neural stem cells comprising an exogenous polynucleotide coding for a growth factor and methods of use thereof
CN116850181A (en) 2015-01-06 2023-10-10 艾尼纳制药公司 Treatment and S1P 1 Methods of receptor-related disorders
BR112017014856A2 (en) 2015-01-08 2018-02-06 Lee Pharma Ltd innovative process for preparation of dipeptidyl peptidase-4 enzyme inhibitor (dpp-4)
CZ27930U1 (en) 2015-01-13 2015-03-10 Zentiva, K.S. Crystalline modification of 3 L-tartrate (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
CZ27898U1 (en) 2015-01-13 2015-03-02 Zentiva, K.S. Crystalline modification of 2 L-tartrate (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4,]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorphenyl)butan-1-one
AU2016229982B2 (en) 2015-03-09 2020-06-18 Intekrin Therapeutics, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
JP2018512436A (en) * 2015-04-15 2018-05-17 バレント・バイオサイエンシーズ・リミテッド・ライアビリティ・カンパニーＶａｌｅｎｔ ＢｉｏＳｃｉｅｎｃｅｓ ＬＬＣ (S) -2'-vinyl-abscisic acid derivative
KR101772898B1 (en) 2015-06-11 2017-08-31 동방에프티엘(주) Improved method of sitagliptin
KR101709127B1 (en) 2015-06-16 2017-02-22 경동제약 주식회사 Novel intermediates for preparing DPP-IV inhibitors, preparing method thereof and preparing method of DPP-IV inhibitors using the same
MX2017016530A (en) 2015-06-22 2018-03-12 Arena Pharm Inc Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluo romethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)a cetic acid(compound1) for use in sipi receptor-associated disorders.
CN105017260B (en) * 2015-07-30 2017-04-19 新发药业有限公司 Preparation method of sitagliptin intermediate triazolopyrazine derivative
WO2017020974A1 (en) 2015-08-03 2017-02-09 Institut Pasteur Dipeptidylpeptidase 4 inhibition enhances lymphocyte trafficking, improving both naturally occurring tumor immunity and immunotherapy
KR20170036288A (en) 2015-09-24 2017-04-03 주식회사 종근당 Novel Salts of Sitagliptin and Preparation Method thereof
WO2017064635A2 (en) 2015-10-14 2017-04-20 Cadila Healthcare Limited Pyrrole compound, compositions and process for preparation thereof
EP3159343B1 (en) * 2015-10-22 2017-07-19 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Improved process for the preparation of triazole and salt thereof
US10450309B2 (en) 2015-11-30 2019-10-22 Merch Sharp & Dohme Corp. Aryl sulfonamides as BLT1 antagonists
US20190382363A1 (en) 2015-11-30 2019-12-19 Merck Sharp & Dohme Corp. Aryl sulfonamides as blt1 antagonists
WO2017201683A1 (en) 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
US10155000B2 (en) 2016-06-10 2018-12-18 Boehringer Ingelheim International Gmbh Medical use of pharmaceutical combination or composition
US10414775B2 (en) 2016-08-15 2019-09-17 Merck Sharp & Dohme Corp. Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
WO2018034918A1 (en) 2016-08-15 2018-02-22 Merck Sharp & Dohme Corp. Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
CN106124667B (en) * 2016-08-29 2018-07-31 上海应用技术学院 A kind of methods of the separation determination Xi Gelieting in relation to substance
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
MX2016016260A (en) 2016-12-08 2018-06-07 Alparis Sa De Cv New solid forms of sitagliptin.
JP6840853B2 (en) 2016-12-09 2021-03-10 カディラ・ヘルスケア・リミテッド Treatment of primary biliary cholangitis
WO2018107415A1 (en) 2016-12-15 2018-06-21 Merck Sharp & Dohme Corp. Hydroxy isoxazole compounds useful as gpr120 agonists
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
US11197949B2 (en) * 2017-01-19 2021-12-14 Medtronic Minimed, Inc. Medication infusion components and systems
US10047094B1 (en) 2017-02-10 2018-08-14 F.I.S.—Fabbrica Italiana Sintetici S.p.A. Process for the preparation of triazole and salt thereof
CN110520124A (en) 2017-02-16 2019-11-29 艾尼纳制药公司 For treating the Compounds and methods for of primary biliary cholangitis
WO2018162722A1 (en) 2017-03-09 2018-09-13 Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Dpp-4 inhibitors for use in treating bone fractures
EP3606527A1 (en) 2017-04-03 2020-02-12 Coherus Biosciences, Inc. Ppar-gamma agonist for treatment of progressive supranuclear palsy
JP7377717B2 (en) 2017-04-24 2023-11-10 ノバルティス アーゲー 2-Amino-L-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-A]pyrazine-7(8H )-il) ethanone and their combination therapeutic regimens
US11096890B2 (en) 2017-09-29 2021-08-24 Merck Sharp & Dohme Corp. Chewable dosage forms containing sitagliptin and metformin
ES2812698T3 (en) 2017-09-29 2021-03-18 Probiodrug Ag Glutaminyl cyclase inhibitors
KR20190060235A (en) 2017-11-24 2019-06-03 제일약품주식회사 Preparation Method Camphorsulfonic acid Salt of Sitagliptin
TR201722603A2 (en) 2017-12-28 2019-07-22 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Tablet formulations comprising metformin and sitagliptin processed with hot-melt extrusion
CN108586346B (en) 2018-05-10 2019-10-01 北京富盛嘉华医药科技有限公司 A kind of method that biocatalysis synthesizes sitagliptin and its intermediate
US11098029B2 (en) 2019-02-13 2021-08-24 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
WO2020205688A1 (en) 2019-04-04 2020-10-08 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
EP4010314B1 (en) 2019-08-08 2024-02-28 Merck Sharp & Dohme LLC Heteroaryl pyrrolidine and piperidine orexin receptor agonists
WO2021076066A1 (en) 2019-10-14 2021-04-22 Santa Farma İlaç Sanayi̇ A.Ş. Oral formulations comprising sitagliptin hci monohydrate with improved pharmaceutical characteristics
KR20210057603A (en) 2019-11-12 2021-05-21 제이투에이치바이오텍 (주) Process for preparing sitagliptin
TW202227417A (en) 2020-08-18 2022-07-16 美商默沙東藥廠 Bicycloheptane pyrrolidine orexin receptor agonists
KR102589305B1 (en) 2021-04-22 2023-10-16 주식회사 메디켐코리아 Improved manufacturing method of sitagliptin phosphate salt
CN113979896A (en) * 2021-11-18 2022-01-28 浙江永太手心医药科技有限公司 Sitagliptin impurity I and preparation method thereof
WO2023139276A1 (en) 2022-01-24 2023-07-27 Zaklady Farmaceutyczne Polpharma S.A. Process for preparing crystalline sitagliptin hydrochloride monohydrate
WO2024086263A1 (en) 2022-10-21 2024-04-25 Merck Sharp & Dohme Llc Compositions of a dipeptidyl peptidase-iv inhibitor and an antioxidant
WO2024121301A1 (en) 2022-12-09 2024-06-13 Krka, D.D., Novo Mesto Process for the preparation of sitagliptin
EP4431087A1 (en) 2023-03-14 2024-09-18 Sanovel Ilac Sanayi Ve Ticaret A.S. A film coated tablet of sitagliptin or a pharmaceutically acceptable salt thereof

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
GB9324803D0 (en) * 1993-12-03 1994-01-19 Ferring Bv Enzyme inhibitors
US5705483A (en) * 1993-12-09 1998-01-06 Eli Lilly And Company Glucagon-like insulinotropic peptides, compositions and methods
AU1856997A (en) 1996-02-02 1997-08-22 Merck & Co., Inc. Method for raising hdl cholesterol levels
US6673927B2 (en) * 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
DE19616486C5 (en) 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Method for lowering the blood glucose level in mammals
AR008789A1 (en) 1996-07-31 2000-02-23 Bayer Corp PIRIDINES AND SUBSTITUTED BIPHENYLS
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
JP2003514508A (en) 1997-07-01 2003-04-15 ノボ ノルディスク アクティーゼルスカブ Glucagon antagonist / adverse agent
US6613942B1 (en) 1997-07-01 2003-09-02 Novo Nordisk A/S Glucagon antagonists/inverse agonists
CN1285834A (en) 1997-11-11 2001-02-28 小野药品工业株式会社 Fused pyrazine compound
US6300314B1 (en) 1998-05-04 2001-10-09 Point Therapeutics, Inc. Hematopoietic stimulation
DE19823831A1 (en) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim New pharmaceutical use of isoleucyl thiazolidide and its salts
DE19828114A1 (en) * 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs of unstable inhibitors of dipeptidyl peptidase IV
FR2780974B1 (en) 1998-07-08 2001-09-28 Sod Conseils Rech Applic USE OF IMIDAZOPYRAZINE DERIVATIVES FOR THE PREPARATION OF A MEDICAMENT FOR TREATING CONDITIONS RESULTING FROM THE FORMATION OF HETEROTRIMETER G PROTEIN
CO5150173A1 (en) 1998-12-10 2002-04-29 Novartis Ag COMPOUNDS N- (REPLACED GLYCLE) -2-DIPEPTIDYL-IV PEPTIDASE INHIBITING CYANOPIRROLIDINS (DPP-IV) WHICH ARE EFFECTIVE IN THE TREATMENT OF CONDITIONS MEDIATED BY DPP-IV INHIBITION
WO2000042026A1 (en) 1999-01-15 2000-07-20 Novo Nordisk A/S Non-peptide glp-1 agonists
GB9906715D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
DE60012721T4 (en) 1999-03-29 2010-09-09 Uutech Ltd., Coleraine ANALOGUE OF THE MAGENTA-INHIBITING PEPTIDE AND ITS USE IN THE TREATMENT OF DIABETES
EP1165519A1 (en) 1999-04-02 2002-01-02 Neurogen Corporation Aryl and heteroaryl fused aminoalkyl-imidazole derivatives and their use as antidiabetics
EP1183229B1 (en) 1999-05-17 2005-10-26 Novo Nordisk A/S Glucagon antagonists/inverse agonists
EP1192182B1 (en) 1999-09-28 2008-06-04 Bayer Corporation Pituitary adenylate cyclase activating peptide (pacap) receptor 3 (r3) agonists and their pharmacological methods of use
AU1916401A (en) 1999-11-12 2001-06-06 Guilford Pharmaceuticals Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
TW583185B (en) 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
JP2004502690A (en) 2000-07-04 2004-01-29 ノボ　ノルディスク　アクティーゼルスカブ Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
UA74912C2 (en) * 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
WO2003082817A2 (en) * 2002-03-25 2003-10-09 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004032836A2 (en) * 2002-10-07 2004-04-22 Merck & Co., Inc. Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors
EP1592689A4 (en) * 2003-01-31 2008-12-24 Merck & Co Inc 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

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